Hypoxia, a state of lower than normal tissue oxygen tension, has recently been implicated in a host of human diseases, including cancer, heart disease, and neurological disorders. An early response to tissue hypoxia is induction of hypoxia inducible factor (HIF), a basic helix-loop-helix (bHLH) PAS (Per/Arnt/Sim) transcriptional factor that mediates changes in gene expression in response to changes in cellular oxygen concentration. HIF is a heterodimer containing an oxygen-regulated alpha subunit (HIF1α) and a constitutively expressed beta subunit (HIFβ), also known as aryl-hydrocarbon receptor nuclear transporter (ARNT). As HIF1 activity has been implicated in numerous disorders, active agents that regulate the activity or stability of HIF1α represent attractive therapeutics for a variety of hypoxia-associated diseases or conditions. Compositions and methods for treating hypoxia-associated diseases or conditions are needed.